5.32384

PI3K Inhibitor, HS-173

• Szinonimák: PI3K Inhibitor, HS-173, PI3Kα Inhibitor, Phosphatidylinositol 3-kinase α Inhibitor
• Tapasztalati képlet (Hill-képlet): C₂₁H₁₈N₄O₄S
• CAS-szám: 1276110-06-5
• Molekulatömeg: 422.46
• MDL-szám: MFCD28023584
• UNSPSC kód: 12352200
• NACRES: NA.77

Tulajdonságok

• Teszt: ≥96% (HPLC)
• Minőségi szint: 100
• Forma: powder
• hatékonyság: 800 pM IC₅₀
• gyártó/kereskedő neve: Calbiochem^®
• tárolási körülmény: OK to freeze; protect from light
• szín: light beige
• oldhatóság: DMSO: 50 mg/mL
• tárolási hőmérséklet: −20°C
• SMILES string: [S](=O)(=O)(Nc2cncc(c2)c3c[n]4c(ncc4C(=O)OCC)cc3)c1ccccc1
• InChI: 1S/C21H18N4O4S/c1-2-29-21(26)19-13-23-20-9-8-15(14-25(19)20)16-10-17(12-22-11-16)24-30(27,28)18-6-4-3-5-7-18/h3-14,24H,2H2,1H3
• Nemzetközi kémiai azonosító kulcs: SEKOTFCHZNXZMM-UHFFFAOYSA-N

Leírás

Általános leírás

A cell permeable imidazopyridine-carboxylate derived compound that acts as a potent and selective inhibitor of phosphatidylinositol 3-kinase a (PI3Ka; IC₅₀ = 800 pM). Blocks the proliferation of several cancer cells (IC₅₀ = 600 nM; 1.5 µM, and 7.8 µM for T47D, SK-BR3, and MCF-7 cells, respectively). Suppresses the growth and proliferation of hepatic stellate cells (HSC-T6 and LX-2 cells) and induces cell cycle arrest at G2/M phase in a dose and time-dependent manner. Induces apoptosis in HSC-T6 cells (~5 µM) as evidenced by morphological changes, activation of caspase-3, reduction in Bcl-2 levels, and loss of mitochondrial transmembrane potential. Exhibits anti-fibrolytic activity and diminishes the expression of profibrotic mediators, such as fibronectin and vimentin (~ 1 µM) and weakens the severity of hepatic damage in a murine model of carbon tetrachloride-induced fibrosis and reduces the phosphorylation of Akt and p70S6 kinase (10 mg/kg, p.o., 6d/week for 1 month).

A cell permeable imidazopyridine-carboxylate derived compound that acts as a potent and selective inhibitor of phosphatidylinositol 3-kinase a (PI3Ka; IC₅₀ = 800 pM). Blocks the proliferation of several cancer cells (IC₅₀ = 600 nM; 1.5 µM, and 7.8 µM for T47D, SK-BR3, and MCF-7 cells, respectively). Suppresses the growth and proliferation of hepatic stellate cells (HSC-T6 and LX-2 cells) and induces cell cycle arrest at G2/M phase in a dose and time-dependent manner. Induces apoptosis in HSC-T6 cells (~5 µM) as evidenced by morphological changes, activation of caspase-3, reduction in Bcl-2 levels, and loss of mitochondrial transmembrane potential. Exhibits anti-fibrolytic activity and diminishes the expression of profibrotic mediators, such as fibronectin and vimentin (~ 1 µM) and weakens the severity of hepatic damage in a murine model of carbon tetrachloride-induced fibrosis and reduces the phosphorylation of Akt and p70S6 kinase (10 mg/kg, p.o., 6d/week for 1 month).

Please note that the molecular weight for this compound is batch-specific due to variable water content.

PI3 K alpha inhibitor; anti-fibrolytic agent; HS-173

Biokémiai/fiziológiai hatások

Cell permeable: yes

Primary Target
PI3Ka

Figyelmeztetés

Toxicity: Standard Handling (A)

Feloldás

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Egyéb megjegyzések

Son, M.K., et al. 2013. Sci. Rep.3, 3470.

Lee, H., et al. 2013. Onc. Rep.30, 863.
Kim, O., et al. 2011. J. Med. Chem.54, 2455.

Jogi információk

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Biztonsági adatok

• Tárolási osztály kódja: 11 - Combustible Solids
• WGK: WGK 3
• Lobbanási pont (F): Not applicable
• Lobbanási pont (C): Not applicable